fg-4592 int 2, cas 1421312-34-6

fg-4592 int 2, cas 1421312-34-6
MF:C18H15NO4
MW:309.32
CAS:1421312-34-6

Synonyms:
ROXA-019
fg-4592 int 2
Fg-4592
FG4592 int 2
4-Hydroxy-1-methyl-7-phenoxy-3-isoquinolinecarboxylic acid methyl ester
Roxadustat intermediate
methyl 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate

The physical properties of fg-4592 int 2, cas 1421312-34-6:
APPearance:White or yellow solid
Density:1.289±0.06 g/cm3
Flash Point:278.7±28.7 °C
Boiling Point:537.3±45.0 °C at 760 mmHg
Vapour Pressure:0.0±1.5 mmHg at 25°C
Index of Refraction:1.646
Acidity coefficient (pKa): 6.24±0.50
Water Solubility:Practically insoluble (0.011 g/L) (25℃)

 

Storage: Sealed in dry,Store in freezer, under -20°C
Application: Intermediates for 808118-40-3; Roxadustat intermediate

Introduction of fg-4592 int 2, cas 1421312-34-6
fg-4592 int 2 is the Intermediates for Roxadustat (FG-4592).Roxadustat (FG-4592) is an HIF-α prolyl hydroxylase inhibitor in a
cell-free assay, stabilizes HIF-2 and induces EPO production.FG-4592 (also known as ASP1517), 2-(4-hydroxy-1-methyl-7-
phenoxyisoquinoline-3-carboxamido)acetic acid, is a potent small molecule inhibitor of hypoxia-inducible factor prolyl hydroxylase
(HIF-PH), an enzyme up-regulating the expression of endogenous human erythropoietin (Epo). It is currently being investigated as an
oral treatment for anemia associated with chronic kidney disease (CKD). Unlike other anemia treating agents, erythropoiesis-
stimulating agents (ESAs), FG-4592 inhibits HIF, through a distinctive mechanism, by stabilization of HIF. According to previous
studies, FG-4592 is capable of correcting and maintaining hemoglobin levels in CKD patients not receiving dialysis and in patients
of end-stage renal disease who receives dialysis but do not need intravenous iron supplement.

Reference:

1. Luis Borges. Different modalities of erythropoiesis stimulating agents. Port J Nephrol Hypert 2010; 24(2): 137-145
2. “FibroGen and Astellas announce initiation of phase 3 trial of FG-4592/ASP1517 for treatment of anemia of chronic kidney disease ” Fibrogen Press Release. Dec 11 2012
3. “FibroGen announces initiation of phase 2b studies of FG-4592, an oral HIF prolyl hydroxylase inhibitor, for treatment of anemia”

Comment

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